ertugliflozin [Ligand Id: 8376] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1770248 (Ertugliflozin, Ertugliflozin l-pyroglutamic acid, Ertugliflozin pidolate, MK-8835, Pf-04971729, PF-04971729, PF04971729, PF-04971729-00, Steglatro) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Low affinity sodium-glucose cotransporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770047] [GtoPdb: 917] [UniProtKB: Q9NY91] | ||||||||
| ChEMBL | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of methyl alpha-D-glucopyranoside uptake after 1 hr | B | 9.06 | pIC50 | 0.88 | nM | IC50 | J Med Chem (2011) 54: 2952-2960 [PMID:21449606] |
| Sodium/glucose cotransporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866] | ||||||||
| ChEMBL | Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of methyl alpha-D-glucopyranoside uptake after 1 hr | B | 5.71 | pIC50 | 1960 | nM | IC50 | J Med Chem (2011) 54: 2952-2960 [PMID:21449606] |
| ChEMBL | Inhibition of human SGLT1 | B | 5.71 | pIC50 | 1960 | nM | IC50 | Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053] |
| GtoPdb | - | - | 5.71 | pIC50 | 1960 | nM | IC50 | J Med Chem (2011) 54: 2952-60 [PMID:21449606] |
| ChEMBL | Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method | B | 6.41 | pIC50 | 392 | nM | IC50 | J Med Chem (2017) 60: 4173-4184 [PMID:28447791] |
| Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639] | ||||||||
| ChEMBL | Inhibition of human SGLT2 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method | B | 8.62 | pIC50 | 2.4 | nM | IC50 | J Med Chem (2017) 60: 4173-4184 [PMID:28447791] |
| ChEMBL | Inhibition of human SGLT2 | B | 9.06 | pIC50 | 0.88 | nM | IC50 | Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053] |
| GtoPdb | - | - | 9.06 | pIC50 | 0.88 | nM | IC50 | J Med Chem (2011) 54: 2952-60 [PMID:21449606] |
| ChEMBL | Inhibition of SGLT2 (unknown origin) | B | 9.06 | pIC50 | 0.87 | nM | IC50 | Medchemcomm (2018) 9: 1273-1281 [PMID:30151080] |
| Sodium/glucose cotransporter 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4316] [GtoPdb: 916] [UniProtKB: P53792] | ||||||||
| ChEMBL | Inhibition of rat SGLT2 | B | 8.94 | pIC50 | 1.15 | nM | IC50 | J Med Chem (2011) 54: 2952-2960 [PMID:21449606] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
